耗材描述
Rubone
产品活性:Rubone 是一种查耳酮类似物,是 miR-34a 的调节剂。Rubone 以 p53 依赖性方式上调 miR-34a 表达,下调下游靶标 Bcl-2 和细胞周期蛋白 D1 表达,并抑制体内肝细胞癌 (HCC) 的生长。Rubone 通过逆转 miR-34a 下游靶标的表达来增强紫杉醇 (PTX; HY-B0015) 在 PTX 耐药的前列腺癌细胞系中的抗癌作用。
产品来源: https://www.medchemexpress.cn/rubone.html
研究领域:Epigenetics
作用靶点:MicroRNA
来源:植物 | 豆科 | 大鱼藤树
结构分类:黄酮类 | 查耳酮 | 结构分类
In Vitro: Rubone (0-60 μM) exhibits significantly high cytotoxicity in DU145-TXR and PC3-TXR cells, suggesting that Rubone has stronger anticancer effect in advanced prostate cancer cells, which has lower miR-34a expression.
Rubone (5, 10 uM; 48 h) significantly reverses the expression of miR-34a downstream gene targets of DU145-TXR and PC3-TXR cell lines.
Rubone (5, 10 uM; 48 h) upregulates miR-34a in PTX-resistant DU145-TXR and PC3-TXR cell lines in a dose dependent manner.
Rubone (5 μM; for 2 weeks) and PTX (for 2 weeks) combination therapy inhibit PC3-TXR cell growth and sphere formation in 3D model, including 3D on top and hanging drop model. Rubone and PTX combination therapy inhibit cell invasion, migration, and cancer stem-like cells (CSCs) population in a p53-independent pathway. Rubone monotherapy or Rubone and PTX combination significantly enhances TAp73 and Elk-1 expression.
In Vivo: Rubone monotherapy (20 mg/kg loaded PEG-PCD micelles; iv for five doses every other day) or combination therapy with PTX (10 mg/kg for each drug loaded PEG-PCD micelles) significantly upregulates miR-34a expression in tumor. The combination therapy inhibits tumor growth. Rubone monotherapy failed to suppress tumor cell proliferation.
相关产品:Camptothecin | Cl-amidine hydrochloride | Diosgenin | Aurintricarboxylic acid | MicroRNA Mimic Negative Control | RGLS4326 | PIN1 inhibitor API-1 | LIN28 inhibitor LI71 | Enoxacin hydrate | MicroRNA Antagomir Negative Control | Targapremir-210 | MicroRNA Inhibitor Negative Control | Pseudoprotodioscin | SID 3712249 | hsa-miR-23a-3p antagomir | hsa-miR-124-3p inhibitor | mmu-miR-155-5p mimic | Cobomarsen | hsa-miR-138-5p agomir | hsa-miR-138-5p antagomir | hsa-miR-146a-5p mimic | hsa-miR-17-5p mimic | hsa-miR-21-5p inhibitor | hsa-miR-21-5p mimic | hsa-miR-26b-5p mimic | hsa-miR-27b-3p mimic | hsa-miR-30c-5p inhibitor | Lin28-let-7a antagonist 1 | MIR96-IN-1 | hsa-miR-106a-3p inhibitor
品牌介绍: MCE (MedChemExpress) 拥有数百种全球独家化合物,我们致力于为全球科研客户提供最新最全的高品质小分子活性化合物;10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域;设有专业的实验中心和严格的质控、验证体系;提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告,确保产品的高纯度、高品质;产品的生物活性多经各国客户实验验证;Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果;专业团队跟踪最新的制药及生命科学研究进展,为您提供全球最新的活性化合物;与世界各大制药公司及知名科研机构建立了长期的合作。